PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
2015 Mar.
Effects of the Ubiquitin Proteasome Inhibitor on Ion Channels in Left Ventricular Hypertrophy and Association of rs3807989 with Atrial Fibrillation
PYR-41 purchased from AbMole
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Source | Int J Med Sci (2018). Figure 5. PYR-41 |
| Method | Western Blotting | |
| Cell Lines | TECs | |
| Concentrations | 0.75 μg/ml | |
| Incubation Time | 24 h | |
| Results | Since RhoT1 is degraded primarily through the ubiquitin proteasome pathway, the ubiquitin-activating enzyme (E1) inhibitor PYR-41 was used to determine whether upregulation of RhoT1 could downregulate the expression of SMAD-4 and promote the expression of JAM-3. |
| Molecular Weight | 371.3 |
| Formula | C17H13N3O7 |
| CAS Number | 418805-02-4 |
| Solubility (25°C) | DMSO 38 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Marina Ikeda, et al. UBE1a Suppresses Herpes Simplex Virus-1 Replication
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